Pentosan polysulfate, pharmaceutical composition, and anticoagulant

Abstract

The present invention provides pentosan polysulfate having a weight average molecular weight of 5000 or less and a content of acetyl groups of 0% to 2.0% by mass, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. The pentosan polysulfate of the present invention, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof exhibits an anti-Xa activity and an anti-Xa/anti-IIa activity ratio, which are suitable for practical use, and is useful as a pharmaceutical composition such as an anticoagulant.

The invention claimed is: 
     
       1. A pentosan polysulfate having a weight average molecular weight of 5000 or less and a content of acetyl groups of 0% to 0.3% by mass, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. 
     
     
       2. The pentosan polysulfate according to  claim 1 , which has a content of acetyl groups of 0% by mass, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. 
     
     
       3. The pentosan polysulfate according to  claim 1 , which has a weight average molecular weight of 4000 or less, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. 
     
     
       4. The pentosan polysulfate according to  claim 1 , which has a structure represented by the following formula, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof: 
       
         
           
           
               
               
           
         
         wherein R each independently represents a hydrogen atom or —SO 3 X 1 , and at least one R is —SO 3 X 1 , wherein X 1  represents a hydrogen atom or a monovalent or divalent metal; X represents a hydrogen atom or a monovalent or divalent metal; and n1 and n2 each independently represent an integer of 0 or more and 15 or less, and at least one of n1 and n2 is an integer of 1 or more. 
       
     
     
       5. The pentosan polysulfate according to  claim 4 , wherein, in Formula 1, X represents sodium, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. 
     
     
       6. The pentosan polysulfate according to  claim 1 , which has a dispersion degree of 1.00 or more and 1.20 or less, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. 
     
     
       7. A pharmaceutical composition comprising, as an active ingredient, the pentosan polysulfate according to  claim 1 , or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof. 
     
     
       8. A method for inhibiting blood coagulation, comprising:
 administrating to a subject in need thereof an effective amount of the pentosan polysulfate according to  claim 1 , or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof.